AU2012244673A1 - Novel binder-drug conjugates (ADCs) and their use - Google Patents

Novel binder-drug conjugates (ADCs) and their use Download PDF

Info

Publication number
AU2012244673A1
AU2012244673A1 AU2012244673A AU2012244673A AU2012244673A1 AU 2012244673 A1 AU2012244673 A1 AU 2012244673A1 AU 2012244673 A AU2012244673 A AU 2012244673A AU 2012244673 A AU2012244673 A AU 2012244673A AU 2012244673 A1 AU2012244673 A1 AU 2012244673A1
Authority
AU
Australia
Prior art keywords
stands
group
denotes
hydrogen
linkage site
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
AU2012244673A
Other languages
English (en)
Inventor
Rudolf Beier
Sandra Borkowski
Sandra Bruder
Sherif El Sheikh
Sven Golfier
Simone Greven
Axel Harrenga
Iring Heisler
Hannah Jorissen
Charotte Christine Kopitz
Hans-Georg Lerchen
Lars Linden
Christoph Mahlert
Heike Petrul
Joachim Schuhmacher
Beatrix Stelte-Ludwig
Karl-Heinz Thierauch
Jorg Willuda
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Seagen Inc
Original Assignee
Bayer Pharma AG
Bayer Intellectual Property GmbH
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bayer Pharma AG, Bayer Intellectual Property GmbH filed Critical Bayer Pharma AG
Publication of AU2012244673A1 publication Critical patent/AU2012244673A1/en
Assigned to SEATTLE GENETICS, INC. reassignment SEATTLE GENETICS, INC. Request for Assignment Assignors: BAYER INTELLECTUAL PROPERTY GMBH, BAYER PHARMA AKTIENGESELLSCHAFT
Abandoned legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/536—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/537—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/68031—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • A61K47/6859—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell the tumour determinant being from liver or pancreas cancer cell
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • A61K47/6869—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell the tumour determinant being from a cell of the reproductive system: ovaria, uterus, testes, prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2812—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2863—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for growth factors, growth regulators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/30—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/20—Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/21—Immunoglobulins specific features characterized by taxonomic origin from primates, e.g. man
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/20—Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/24—Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/56—Immunoglobulins specific features characterized by immunoglobulin fragments variable (Fv) region, i.e. VH and/or VL
    • C07K2317/565—Complementarity determining region [CDR]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/70—Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
    • C07K2317/76—Antagonist effect on antigen, e.g. neutralization or inhibition of binding

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Cell Biology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Reproductive Health (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
AU2012244673A 2011-04-21 2012-04-20 Novel binder-drug conjugates (ADCs) and their use Abandoned AU2012244673A1 (en)

Applications Claiming Priority (25)

Application Number Priority Date Filing Date Title
EP11163474 2011-04-21
EP11163467.1 2011-04-21
EP11163470.5 2011-04-21
EP11163470 2011-04-21
EP11163474.7 2011-04-21
EP11163467 2011-04-21
EP11163472.1 2011-04-21
EP11163472 2011-04-21
EP11168558 2011-06-01
EP11168556 2011-06-01
EP11168557 2011-06-01
EP11168557.4 2011-06-01
EP11168556.6 2011-06-01
EP11168558.2 2011-06-01
EP11168559.0 2011-06-01
EP11168559 2011-06-01
EP11193623.3 2011-12-14
EP11193621.7 2011-12-14
EP11193609.2 2011-12-14
EP11193609 2011-12-14
EP11193618 2011-12-14
EP11193618.3 2011-12-14
EP11193621 2011-12-14
EP11193623 2011-12-14
PCT/EP2012/057243 WO2012143495A2 (de) 2011-04-21 2012-04-20 Neue binder-wirkstoff konjugate (adcs) und ihre verwendung

Publications (1)

Publication Number Publication Date
AU2012244673A1 true AU2012244673A1 (en) 2013-11-28

Family

ID=45976407

Family Applications (3)

Application Number Title Priority Date Filing Date
AU2012244673A Abandoned AU2012244673A1 (en) 2011-04-21 2012-04-20 Novel binder-drug conjugates (ADCs) and their use
AU2012244675A Ceased AU2012244675B2 (en) 2011-04-21 2012-04-20 Novel binder-drug conjugates (ADCs) and their use
AU2017203928A Ceased AU2017203928B2 (en) 2011-04-21 2017-06-09 Novel binder-drug conjugates (ADCs) and their use

Family Applications After (2)

Application Number Title Priority Date Filing Date
AU2012244675A Ceased AU2012244675B2 (en) 2011-04-21 2012-04-20 Novel binder-drug conjugates (ADCs) and their use
AU2017203928A Ceased AU2017203928B2 (en) 2011-04-21 2017-06-09 Novel binder-drug conjugates (ADCs) and their use

Country Status (16)

Country Link
US (7) US20130122024A1 (enExample)
EP (2) EP2699268A2 (enExample)
JP (3) JP6088488B2 (enExample)
KR (2) KR20140122649A (enExample)
CN (3) CN103764170A (enExample)
AR (2) AR086363A1 (enExample)
AU (3) AU2012244673A1 (enExample)
BR (1) BR112013027119A8 (enExample)
CA (3) CA2833690A1 (enExample)
IL (2) IL228841A (enExample)
MX (1) MX2013012253A (enExample)
RU (2) RU2610336C2 (enExample)
SG (2) SG194567A1 (enExample)
TW (2) TWI582112B (enExample)
WO (4) WO2012143499A2 (enExample)
ZA (1) ZA201307955B (enExample)

Families Citing this family (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR076284A1 (es) 2009-04-29 2011-06-01 Bayer Schering Pharma Ag Inmunoconjugados de antimesotelina y usos de los mismos
AU2010329904B2 (en) * 2009-12-09 2015-07-09 Bayer Pharma Aktiengesellschaft Anti-C4.4a antibodies and uses thereof
WO2011154359A1 (de) * 2010-06-10 2011-12-15 Bayer Pharma Aktiengesellschaft Neue auristatin-derivate und ihre verwendung
JP5933562B2 (ja) 2010-09-29 2016-06-15 シアトル ジェネティックス， インコーポレイテッド Ｎ−カルボキシアルキル−アウリスタチンおよびその使用
US9029406B2 (en) 2011-03-16 2015-05-12 Seattle Genetics, Inc N-carboxyalkylauristatins and use thereof
BR112013027119A8 (pt) * 2011-04-21 2018-03-06 Seattle Genetics Inc novos conjugados ligante-droga (adcs) e uso dos mesmos
SG11201403085PA (en) * 2011-12-14 2014-10-30 Seattle Genetics Inc Fgfr antibody drug conjugates (adcs) and the use thereof
WO2014093379A1 (en) 2012-12-10 2014-06-19 Mersana Therapeutics, Inc. Auristatin compounds and conjugates thereof
EP2927227A4 (en) * 2013-01-03 2015-12-30 Celltrion Inc ANTIBODY CONCENTRATOR REMEDY CONJUGATE, METHOD OF MANUFACTURING THEREOF, AND ANTIBODY TOGETHER THEREWITH
HK1220626A1 (zh) 2013-03-15 2017-05-12 The Centre For Drug Research And Development 具细胞毒性和抗有丝分裂的化合物以及其使用方法
FR3005051A1 (fr) * 2013-04-25 2014-10-31 Pf Medicament Derives de la dolastatine 10 et d'auristatines
KR20160018579A (ko) * 2013-06-04 2016-02-17 싸이톰스 테라퓨틱스, 인크. 활성화가능 항체를 접합하기 위한 조성물 및 방법
WO2015059147A1 (en) * 2013-10-25 2015-04-30 Bayer Pharma Aktiengesellschaft A novel stable formulation
JP6671292B2 (ja) * 2013-12-16 2020-03-25 ジェネンテック， インコーポレイテッド ペプチド模倣化合物及びその抗体−薬物コンジュゲート
JP6636925B2 (ja) 2013-12-17 2020-01-29 ノバルティス アーゲー 細胞障害性ペプチドおよびその抱合体
RU2698697C2 (ru) 2013-12-23 2019-08-29 Байер Фарма Акциенгезельшафт Конъюгаты связующего (ADC) с ингибиторами KSP
WO2015095953A1 (en) 2013-12-27 2015-07-02 The Centre For Drug Research And Development Sulfonamide-containing linkage systems for drug conjugates
BR112016015105A8 (pt) 2013-12-27 2018-04-24 Var2 Pharmaceuticals Aps conjugados var2csa-droga
US10464955B2 (en) 2014-02-28 2019-11-05 Hangzhou Dac Biotech Co., Ltd. Charged linkers and their uses for conjugation
US9260478B2 (en) 2014-04-04 2016-02-16 Shanghui Hu Potent and efficient cytotoxic peptides and antibody-drug conjugates thereof and their synthesis
WO2015183978A1 (en) * 2014-05-28 2015-12-03 Agensys, Inc. Derivatives of dolaproine-dolaisoleuine peptides
CA2951368A1 (en) 2014-06-13 2015-12-17 Novartis Ag Auristatin derivatives and conjugates thereof
ES2905569T3 (es) 2014-09-17 2022-04-11 Zymeworks Inc Compuestos citotóxicos y antimitóticos y métodos para utilizarlos
CN105820248A (zh) * 2015-01-07 2016-08-03 上海张江生物技术有限公司 一种新型抗egfr单克隆抗体的制备方法及应用
WO2016127790A1 (zh) * 2015-02-15 2016-08-18 江苏恒瑞医药股份有限公司 配体-细胞毒性药物偶联物、其制备方法及其应用
PT3271329T (pt) 2015-03-19 2021-10-25 Hangzhou Dac Biotech Co Ltd Novos ligantes hidrofílicos e conjugados ligando-fármaco dos mesmos
AU2016249839B2 (en) 2015-04-17 2021-09-09 Ventana Medical Systems, Inc. Antibodies, compositions, and immunohistochemistry methods for detecting C4.4a
US10526287B2 (en) 2015-04-23 2020-01-07 Constellation Pharmaceuticals, Inc. LSD1 inhibitors and uses thereof
WO2015151079A2 (en) * 2015-06-20 2015-10-08 Hangzhou Dac Biotech Co, Ltd Auristatin analogues and their conjugates with cell-binding molecules
JP6971858B2 (ja) 2015-06-22 2021-11-24 バイエル ファーマ アクチエンゲゼルシャフト 酵素開裂性基を有する抗体薬物複合体（ａｄｃ）および抗体プロドラッグ複合体（ａｐｄｃ）
US10435435B2 (en) * 2015-07-24 2019-10-08 The Arizona Board Of Regents On Behalf Of Arizona State University Quinstatin compounds
WO2017058808A1 (en) 2015-10-02 2017-04-06 Sirenas Llc Anti-cancer compounds and conjugates thereof
WO2017060322A2 (en) 2015-10-10 2017-04-13 Bayer Pharma Aktiengesellschaft Ptefb-inhibitor-adc
CA3015098A1 (en) 2016-02-26 2017-08-31 Jiangsu Hengrui Medicine Co., Ltd. New toxin and method for preparing intermediate thereof
WO2017161206A1 (en) 2016-03-16 2017-09-21 Halozyme, Inc. Conjugates containing conditionally active antibodies or antigen-binding fragments thereof, and methods of use
JP7251981B2 (ja) 2016-03-24 2023-04-04 バイエル ファーマ アクチエンゲゼルシャフト 酵素開裂基を有する細胞毒性活性剤のプロドラッグ
EP3919518A1 (en) 2016-06-15 2021-12-08 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies
WO2018006785A1 (zh) * 2016-07-05 2018-01-11 江苏恒瑞医药股份有限公司 Egfr抗体-药物偶联物及其在医药上的应用
US10517958B2 (en) 2016-10-04 2019-12-31 Zymeworks Inc. Compositions and methods for the treatment of platinum-drug resistant cancer
TWI753037B (zh) 2016-10-26 2022-01-21 美商星座製藥公司 Lsd1抑制劑及其用途
EP3554544A4 (en) 2016-12-16 2020-07-29 Bluefin Biomedicine, Inc. ANTI-PROTEIN 1 ANTIBODY CONTAINING AN ANTI-CUB DOMAIN (CDCP1), ANTIBODY-DRUG CONJUGATES AND THEIR METHODS OF USE
CN110072556B (zh) 2016-12-21 2023-05-02 拜耳制药股份公司 具有ksp抑制剂的特异性抗体药物缀合物(adc)
CN110312534B (zh) 2016-12-21 2023-04-04 拜耳制药股份公司 具有酶促可裂解基团的抗体-药物-缀合物(adc)
US12059472B2 (en) 2016-12-21 2024-08-13 Bayer Aktiengesellschaft Prodrugs of cytotoxic active agents having enzymatically cleavable groups
ES2973548T3 (es) 2016-12-22 2024-06-20 Cue Biopharma Inc Polipéptidos multiméricos moduladores de linfocitos T y métodos para su uso
KR20210122319A (ko) * 2017-04-06 2021-10-08 항저우 디에이씨 바이오테크 씨오, 엘티디 비스-링키지를 사용한 세포독성 약물의 접합
JP7298926B2 (ja) * 2017-07-12 2023-06-27 ノイスコム アーゲー 癌の治療のためのネオアンチゲンワクチン組成物
US10646585B2 (en) 2017-09-15 2020-05-12 Hangzhou Dac Biotech Co., Ltd. Hydrophilic linkers and ligand-drug conjugates thereof
CN107998453B (zh) * 2017-12-12 2020-09-25 中山大学附属第一医院 一种表面改性的脱细胞基质及其改性方法
GB201721265D0 (en) * 2017-12-19 2018-01-31 Bicyclerd Ltd Bicyclic peptide ligands specific for EphA2
EP3746079A1 (en) 2018-01-31 2020-12-09 Bayer Aktiengesellschaft Antibody drug conjugates (adcs) with nampt inhibitors
TW202003047A (zh) 2018-03-23 2020-01-16 美商西雅圖遺傳學公司 包括微管蛋白破壞劑之抗體藥物結合物治療實體腫瘤之用途
WO2021013693A1 (en) 2019-07-23 2021-01-28 Bayer Pharma Aktiengesellschaft Antibody drug conjugates (adcs) with nampt inhibitors
EP4054602A4 (en) 2019-11-08 2023-12-06 Mayo Foundation for Medical Education and Research EPHA3 TARGETED CAR-T CELLS FOR TREATING TUMORS
EP4087855A1 (en) * 2020-01-06 2022-11-16 CytomX Therapeutics, Inc. Auristatin-related compounds, conjugated auristatin-related compounds, and methods of use thereof
WO2021231376A2 (en) 2020-05-12 2021-11-18 Cue Biopharma, Inc. Multimeric t-cell modulatory polypeptides and methods of use thereof
CN116669772A (zh) * 2020-11-19 2023-08-29 艾迪健公司 Gpc3结合剂、其缀合物以及使用它们的方法
WO2022105878A1 (en) * 2020-11-20 2022-05-27 Bliss Biopharmaceutical (Hangzhou) Co., Ltd. Modified egfr antibody with reduced affinity, drug conjugate, and use thereof
WO2022216848A1 (en) * 2021-04-06 2022-10-13 Hemoshear Therapeutics, Inc. Methods of treating methylmalonic acidemia and propionic acidemia
CN118119409A (zh) 2021-09-03 2024-05-31 东丽株式会社 癌的治疗和/或预防用药物组合物
WO2023061405A1 (zh) * 2021-10-12 2023-04-20 成都科岭源医药技术有限公司 一种高稳定性的靶向接头-药物偶联物
WO2023092099A1 (en) 2021-11-19 2023-05-25 Ardeagen Corporation Gpc3 binding agents, conjugates thereof and methods of using the same
CN114149343B (zh) * 2021-12-06 2023-10-20 中节能万润股份有限公司 一种高纯度1,4-二氰基-2-丁烯的制备方法
CA3258344A1 (en) 2022-06-07 2023-12-14 Actinium Pharmaceuticals, Inc. CHELETARIANS AND BIFUNCTIONAL CONJUGATES
CA3258612A1 (en) * 2022-06-09 2023-12-14 Beigene, Ltd. Antibody drug conjugates
TW202412762A (zh) * 2022-07-27 2024-04-01 香港商祐方有限公司 奧瑞他汀衍生物及其結合物
TW202434307A (zh) 2023-01-18 2024-09-01 大陸商泰勵生物科技（上海）有限公司 抗體偶聯藥物及其用途
CN116239513B (zh) * 2023-05-05 2023-08-18 天津凯莱英制药有限公司 Mmae关键中间体的制备方法、mmae的制备方法和抗体偶联药物
US20260048137A1 (en) 2024-08-16 2026-02-19 Ardeagen Corporation Anti-mesothelin antibody conjugates and methods of use thereof

Family Cites Families (107)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1981003688A1 (en) 1980-06-13 1981-12-24 Crosby Valve & Eng Co Ltd Fluid pressure relief system actuator
FR2499737B1 (fr) 1981-02-12 1985-07-05 Laudren Cie Sa Ets M Circuit d'alarme pour systemes de surveillance de postes telephoniques publics a prepaiement
US4474893A (en) 1981-07-01 1984-10-02 The University of Texas System Cancer Center Recombinant monoclonal antibodies
US4714681A (en) 1981-07-01 1987-12-22 The Board Of Reagents, The University Of Texas System Cancer Center Quadroma cells and trioma cells and methods for the production of same
EP0071286B1 (en) 1981-07-30 1985-08-28 Shell Internationale Researchmaatschappij B.V. Process for the preparation of carbonate esters
DE3223868A1 (de) 1982-06-25 1983-12-29 Friedrich 8541 Röttenbach Schweinfurter Turbinenpumpe
HUT36107A (en) 1982-12-04 1985-08-28 Lilly Industries Ltd Process for production of new aurone-derivatives and medical preparatives consisting of such compounds
GB8308235D0 (en) 1983-03-25 1983-05-05 Celltech Ltd Polypeptides
US4816567A (en) 1983-04-08 1989-03-28 Genentech, Inc. Recombinant immunoglobin preparations
GB2163883B (en) 1984-08-29 1989-02-01 British Aerospace Data processing arrangement
FR2576708B1 (fr) 1985-01-25 1987-04-30 Novatome Generateur de vapeur dont le fluide caloporteur est du metal liquide et dont la detection des fuites est effectuee par prelevement de ce metal liquide
US4606662A (en) 1985-01-31 1986-08-19 International Business Machines Corporation Single stepping motor ribbon and correction feed and lift system
US4640839A (en) 1985-07-01 1987-02-03 Nestec S.A. Agglomeration process
DE8808645U1 (de) 1988-07-06 1988-08-25 Hofer, Daniel, 7730 Villingen-Schwenningen Anzeigeeinrichtung für Feuerlöscher
US4925648A (en) 1988-07-29 1990-05-15 Immunomedics, Inc. Detection and treatment of infectious and inflammatory lesions
US5601819A (en) 1988-08-11 1997-02-11 The General Hospital Corporation Bispecific antibodies for selective immune regulation and for selective immune cell binding
ES2096590T3 (es) 1989-06-29 1997-03-16 Medarex Inc Reactivos biespecificos para la terapia del sida.
ES2133139T3 (es) 1989-10-20 1999-09-01 Medarex Inc Hetero anticuerpos biespecificos con funciones efectoras dobles.
US5270163A (en) 1990-06-11 1993-12-14 University Research Corporation Methods for identifying nucleic acid ligands
DK0553244T4 (da) 1990-10-05 2005-08-01 Celldex Therapeutics Inc Målrettet immunostimulering med bispecifikke reagenser
WO1992008802A1 (en) 1990-10-29 1992-05-29 Cetus Oncology Corporation Bispecific antibodies, method of production, and uses thereof
CA2082160C (en) 1991-03-06 2003-05-06 Mary M. Bendig Humanised and chimeric monoclonal antibodies
CA2108451A1 (en) 1991-04-26 1992-10-27 Beverley J. Randle Novel antibodies, and methods for their use
PT627940E (pt) 1992-03-05 2003-07-31 Univ Texas Utilizacao de imunoconjugados para o diagnostico e/ou terapia de tumores vascularizados
EP0719859B1 (en) 1994-12-20 2003-07-02 MERCK PATENT GmbH Anti-alpha V-integrin monoclonal antibody
ES2176484T3 (es) 1995-08-18 2002-12-01 Morphosys Ag Bancos de proteinas/(poli)peptidos.
US6150508A (en) 1996-03-25 2000-11-21 Northwest Biotherapeutics, Inc. Monoclonal antibodies specific for the extracellular domain of prostate-specific membrane antigen
EP0914155B1 (en) 1996-03-25 2006-02-22 Medarex, Inc. Monoclonal antibodies specific for the extracellular domain of prostate specific membrane antigen
WO2000003737A2 (en) * 1998-07-17 2000-01-27 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Water-soluble drugs and methods for their production
CZ20014083A3 (cs) 1999-05-14 2002-08-14 Imclone Systems Incorporated Léčivo pro indikaci růstu refrakterních nádorů
CA2370245A1 (en) 1999-05-14 2000-11-23 Boehringer Ingelheim Pharmaceuticals, Inc. Enzyme-activated anti-tumor prodrug compounds
NZ517331A (en) 1999-07-29 2004-02-27 Medarex Inc Human monoclonal antibodies to prostate specific membrane antigen and a transgenic mouse to produce the antibody
US6323315B1 (en) 1999-09-10 2001-11-27 Basf Aktiengesellschaft Dolastatin peptides
EP1220919A2 (en) 1999-09-29 2002-07-10 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts Metastasis-associated antigen c4.4a
ATE419354T1 (de) 2000-02-25 2009-01-15 Us Gov Health & Human Serv Scfv-moleküle gegen egfrviii mit verbesserter zytotoxizität und ausbeute, darauf basierte immuntoxine, und verfahren zur deren verwendung
BR0110927A (pt) 2000-05-19 2003-03-11 Scancell Ltd Anticorpo, ácido nucléico, vetor, célula, método de fabricar um anticorpo, composição farmacêutica, uso de um anticorpo ou de um ácido nucleico, e, método para o tratamento ou profilaxia do câncer
US7288390B2 (en) 2000-08-07 2007-10-30 Centocor, Inc. Anti-dual integrin antibodies, compositions, methods and uses
AUPR395801A0 (en) 2001-03-26 2001-04-26 Austin Research Institute, The Antibodies against cancer
PL207087B1 (pl) 2001-04-26 2010-10-29 Biogen Przeciwciało, które wiąże się swoiście z białkiem Cripto, zawierająca je kompozycja farmaceutyczna i zastosowanie przeciwciała
US6884869B2 (en) 2001-04-30 2005-04-26 Seattle Genetics, Inc. Pentapeptide compounds and uses related thereto
AU2002311919B8 (en) 2001-05-11 2007-03-22 Ludwig Institute For Cancer Research Ltd Specific binding proteins and uses thereof
US7595378B2 (en) 2001-06-13 2009-09-29 Genmab A/S Human monoclonal antibodies to epidermal growth factor receptor (EGFR)
CA2450285C (en) 2001-06-13 2016-08-02 Genmab A/S Human monoclonal antibodies to epidermal growth factor receptor (egfr)
WO2003026577A2 (en) 2001-09-24 2003-04-03 Seattle Genetics, Inc. P-amidobenzylethers in drug delivery agents
US7091186B2 (en) 2001-09-24 2006-08-15 Seattle Genetics, Inc. p-Amidobenzylethers in drug delivery agents
NZ535425A (en) 2002-03-13 2008-05-30 Biogen Idec Inc Anti-alphavbeta6 antibodies
JP2005520566A (ja) 2002-03-22 2005-07-14 バイオジェン・アイデック・エムエイ・インコーポレイテッド Ｃｒｉｐｔｏ特異的抗体
ES2524767T3 (es) 2002-06-14 2014-12-12 Immunomedics, Inc. Anticuerpo monoclonal humanizado HPAM4
DK1545613T3 (da) 2002-07-31 2011-11-14 Seattle Genetics Inc Auristatinkonjugater og deres anvendelse til behandling af cancer, en autoimmun sygdom eller en infektiøs sygdom
WO2004091375A2 (en) 2003-04-11 2004-10-28 Medimmune, Inc. Epha2 and non-neoplastic hyperproliferative cell disorders
KR20130065723A (ko) 2003-06-27 2013-06-19 암젠 프레몬트 인코포레이티드 상피 성장 인자 수용체의 결실 돌연변이체 지향 항체 및 그 용도
ATE496944T1 (de) 2003-07-21 2011-02-15 Immunogen Inc Ca6-antigenspezifisches zytotoxisches konjugat und verfahren zu dessen anwendung
EP2478912B1 (en) * 2003-11-06 2016-08-31 Seattle Genetics, Inc. Auristatin conjugates with anti-HER2 or anti-CD22 antibodies and their use in therapy
EP1701979A2 (en) 2003-12-03 2006-09-20 Xencor, Inc. Optimized antibodies that target the epidermal growth factor receptor
US7767792B2 (en) 2004-02-20 2010-08-03 Ludwig Institute For Cancer Research Ltd. Antibodies to EGF receptor epitope peptides
CA2560305C (en) 2004-03-19 2016-07-05 Imclone Systems Incorporated Human anti-epidermal growth factor receptor antibody
WO2005101017A1 (en) * 2004-04-07 2005-10-27 Genentech, Inc. Mass spectrometry of antibody conjugates
MX2007003907A (es) * 2004-10-05 2007-05-21 Genentech Inc Agentes terapeuticos con toxicidad reducida.
US8288352B2 (en) 2004-11-12 2012-10-16 Seattle Genetics, Inc. Auristatins having an aminobenzoic acid unit at the N terminus
DE602005022928D1 (de) * 2004-11-30 2010-09-23 Abgenix Inc Antikörper gegen gpnmb und ihre verwendungen
US8603483B2 (en) 2004-12-09 2013-12-10 Janssen Biotech, Inc. Anti-integrin immunoconjugates, methods and uses
EP2230517A1 (en) 2005-01-07 2010-09-22 Diadexus, Inc. OVR110 antibody compositions and methods of use
ES2498794T3 (es) 2005-02-18 2014-09-25 Medarex, L.L.C. Anticuerpos monoclonales contra CD30 que carecen de restos fucosilo
ES2708763T3 (es) 2005-07-07 2019-04-11 Seattle Genetics Inc Compuestos de monometilvalina que tienen modificaciones de la cadena lateral de fenilalanina en el extremo C
WO2007008848A2 (en) 2005-07-07 2007-01-18 Seattle Genetics, Inc. Monomethylvaline compounds having phenylalanine carboxy modifications at the c-terminus
CA3000520C (en) 2005-08-24 2023-04-04 Immunogen, Inc. Process for preparing antibody maytansinoid conjugates
EP1928912A4 (en) * 2005-09-07 2010-02-24 Medimmune Inc EPH ANTI-RECEPTOR ANTIBODIES CONJUGATED TO TOXINS
NZ566395A (en) 2005-09-26 2012-03-30 Medarex Inc Human monoclonal antibodies to CD70
EP1957115B8 (en) * 2005-11-10 2014-03-05 Celldex Therapeutics, Inc. Method of treating ovarian and renal cancer using antibodies against t cell immunoglobulin domain and mucin domain 1 (tim-1) antigen
DOP2006000277A (es) 2005-12-12 2007-08-31 Bayer Pharmaceuticals Corp Anticuerpos anti mn y métodos para su utilización
EP2032606B1 (en) * 2006-05-30 2013-11-27 Genentech, Inc. Antibodies and immunoconjugates and uses therefor
WO2008004834A1 (en) 2006-07-06 2008-01-10 Isu Abxis Co., Ltd Humanized monoclonal antibody highly binding to epidermal growth factor receptor, egf receptor
RU2495882C2 (ru) 2006-09-08 2013-10-20 Медиммун, Ллк. Гуманизированные антитела к cd19 и их применение для лечения онкологического, связанного с трансплантацией и аутоиммунного заболевания
EP3539981A1 (en) 2006-09-10 2019-09-18 Glycotope GmbH Use of human cells of myeloid leukaemia origin for expression of antibodies
WO2008036688A2 (en) 2006-09-18 2008-03-27 Xencor, Inc. Optimized antibodies that target hm1.24
WO2008133641A2 (en) * 2006-10-11 2008-11-06 Curagen Corporation Antibodies directed to gpnmb and uses thereof
EP1914242A1 (en) 2006-10-19 2008-04-23 Sanofi-Aventis Novel anti-CD38 antibodies for the treatment of cancer
PT2099823E (pt) 2006-12-01 2014-12-22 Seattle Genetics Inc Agentes de ligação ao alvo variantes e suas utilizações
US8652466B2 (en) 2006-12-08 2014-02-18 Macrogenics, Inc. Methods for the treatment of disease using immunoglobulins having Fc regions with altered affinities for FcγRactivating and FcγRinhibiting
WO2008092117A2 (en) 2007-01-25 2008-07-31 Xencor, Inc. Immunoglobulins with modifications in the fcr binding region
CN108424454B (zh) 2007-08-14 2022-05-31 路德维格癌症研究所有限公司 靶向egf受体的单克隆抗体175及其衍生物和用途
US8865875B2 (en) 2007-08-22 2014-10-21 Medarex, L.L.C. Site-specific attachment of drugs or other agents to engineered antibodies with C-terminal extensions
PT2185574E (pt) 2007-09-07 2013-08-26 Agensys Inc Anticorpos e moléculas relacionadas que se ligam a proteínas 24p4c12
US8039597B2 (en) 2007-09-07 2011-10-18 Agensys, Inc. Antibodies and related molecules that bind to 24P4C12 proteins
ES2526355T3 (es) * 2007-10-01 2015-01-09 Bristol-Myers Squibb Company Anticuerpos humanos que se adhieren a mesotelina, y usos de los mismos
MX2010005603A (es) 2007-11-26 2010-08-02 Bayer Schering Pharma Ag Anticuerpos antimesotelina y usos de los mismos.
US9221914B2 (en) 2007-12-26 2015-12-29 Biotest Ag Agents targeting CD138 and uses thereof
CN101965366B (zh) 2007-12-26 2016-04-27 生物测试股份公司 靶向cd138的免疫缀合物及其应用
KR101607346B1 (ko) * 2008-01-31 2016-03-29 제넨테크, 인크. 항-ｃｄ７９ｂ 항체 및 면역접합체 및 사용 방법
US20110126727A1 (en) 2008-02-25 2011-06-02 Prittie Allan R Raised Image Plate Construction with Regions of Varying Support Thickness Beneath the Image Areas
EP2260111B2 (en) * 2008-03-14 2022-03-23 Genentech, Inc. Genetic variations associated with drug resistance
DK2265283T3 (da) 2008-03-18 2014-10-20 Seattle Genetics Inc Auristatin-lægemiddel-linker-konjugater
WO2009123894A2 (en) 2008-04-02 2009-10-08 Macrogenics, Inc. Her2/neu-specific antibodies and methods of using same
WO2009140242A1 (en) * 2008-05-13 2009-11-19 Genentech, Inc. Analysis of antibody drug conjugates by bead-based affinity capture and mass spectrometry
WO2010022736A2 (en) 2008-08-29 2010-03-04 Symphogen A/S Recombinant anti-epidermal growth factor receptor antibody compositions
US20100247484A1 (en) 2009-03-31 2010-09-30 Heinrich Barchet Combination therapy of an afucosylated antibody and one or more of the cytokines gm csf, m csf and/or il3
CA2754646A1 (en) 2009-03-31 2010-10-07 Roche Glycart Ag Treatment of cancer with a humanized anti-egfr igg1 antibody and irinotecan
MX2011013578A (es) 2009-06-19 2012-01-20 Merck Patent Gmbh Biomarcadores y metodos para determinar la eficacia de anticuerpos anti-receptor del factor de crecimiento epidermal (anti-egfr) en terapia de cancer.
JP5898082B2 (ja) 2009-10-07 2016-04-06 マクロジェニクス，インコーポレーテッド フコシル化程度の変更により改良されたエフェクター機能を示すＦｃ領域含有ポリペプチドおよびその使用法
AU2010329904B2 (en) 2009-12-09 2015-07-09 Bayer Pharma Aktiengesellschaft Anti-C4.4a antibodies and uses thereof
WO2011154359A1 (de) * 2010-06-10 2011-12-15 Bayer Pharma Aktiengesellschaft Neue auristatin-derivate und ihre verwendung
JP5933562B2 (ja) * 2010-09-29 2016-06-15 シアトル ジェネティックス， インコーポレイテッド Ｎ−カルボキシアルキル−アウリスタチンおよびその使用
BR112013014527A2 (pt) * 2010-12-20 2017-03-07 Genentech Inc anticorpo isolado, ácido nucleico isolado, célula hospedeira, método para produzir um anticorpo, imunoconjugado, formulação farmacêutica, uso do imunoconjugado, método para tratamento de um indivíduo que tem um câncer positivo para mesotelina, para inibição de proliferação de uma célula positiva para mesotelina, para detecção de mesotelina humana em uma amostra biológica e para detectar um câncer positivo para mesotelina
US9302799B2 (en) * 2011-02-17 2016-04-05 Sabic Global Technologies B.V. Method for bulk transporting 2,6-xylenol susceptible to oxidative discoloration
US9029406B2 (en) 2011-03-16 2015-05-12 Seattle Genetics, Inc N-carboxyalkylauristatins and use thereof
BR112013027119A8 (pt) 2011-04-21 2018-03-06 Seattle Genetics Inc novos conjugados ligante-droga (adcs) e uso dos mesmos
SG11201403085PA (en) 2011-12-14 2014-10-30 Seattle Genetics Inc Fgfr antibody drug conjugates (adcs) and the use thereof

Also Published As

Publication number Publication date
TW201305218A (zh) 2013-02-01
CN103764170A (zh) 2014-04-30
CN103826661B (zh) 2019-03-05
US20140127240A1 (en) 2014-05-08
EP3501546A2 (de) 2019-06-26
TW201722483A (zh) 2017-07-01
US20130066055A1 (en) 2013-03-14
KR20140122167A (ko) 2014-10-17
EP3501546A3 (de) 2019-09-18
US20160193359A1 (en) 2016-07-07
AU2012244675A1 (en) 2013-11-28
BR112013027119A2 (pt) 2017-09-26
WO2012143499A3 (de) 2012-12-13
US8992932B2 (en) 2015-03-31
US20150246136A1 (en) 2015-09-03
RU2013151599A (ru) 2015-05-27
WO2012143497A3 (de) 2013-03-21
SG10201702384PA (en) 2017-05-30
NZ615839A (en) 2015-11-27
JP2014512375A (ja) 2014-05-22
CA3027793A1 (en) 2012-10-26
WO2012143496A2 (de) 2012-10-26
IL228841A0 (en) 2013-12-31
TWI636793B (zh) 2018-10-01
AR086364A1 (es) 2013-12-11
TWI582112B (zh) 2017-05-11
WO2012143495A3 (de) 2012-12-13
RU2610336C2 (ru) 2017-02-09
WO2012143497A2 (de) 2012-10-26
US20150030618A1 (en) 2015-01-29
CN103826661A (zh) 2014-05-28
IL228841A (en) 2017-07-31
JP6250735B2 (ja) 2017-12-20
SG194567A1 (en) 2013-12-30
US20130122024A1 (en) 2013-05-16
AR086363A1 (es) 2013-12-11
JP6088488B2 (ja) 2017-03-01
CA2833690A1 (en) 2012-10-26
KR20140122649A (ko) 2014-10-20
JP2016175941A (ja) 2016-10-06
JP2014515753A (ja) 2014-07-03
RU2013151600A (ru) 2015-05-27
KR102023496B1 (ko) 2019-09-20
MX2013012253A (es) 2014-02-17
IL248036B (en) 2018-04-30
BR112013027119A8 (pt) 2018-03-06
AU2017203928A1 (en) 2017-07-06
EP2699268A2 (de) 2014-02-26
WO2012143499A2 (de) 2012-10-26
WO2012143495A2 (de) 2012-10-26
WO2012143496A3 (de) 2013-03-21
AU2012244675B2 (en) 2017-06-29
US20130095123A1 (en) 2013-04-18
AU2017203928B2 (en) 2019-02-21
ZA201307955B (en) 2015-01-28
CA2833477A1 (en) 2012-10-26
CN106117312A (zh) 2016-11-16

Similar Documents

Publication Publication Date Title
AU2017203928B2 (en) Novel binder-drug conjugates (ADCs) and their use
CN110312534B (zh) 具有酶促可裂解基团的抗体-药物-缀合物(adc)
US20150023989A1 (en) New antibody drug conjugates (adcs) and the use thereof
KR20190099250A (ko) 효소적으로 절단가능한 기를 갖는 세포독성 활성제의 전구약물
NZ615839B2 (en) Novel binder-drug conjugates (adcs) and their use
NZ625745B2 (en) FGFR antibody drug conjugates (ADCs) and the use thereof
TW201302799A (zh) 新穎結合劑－藥物接合物（ＡＤＣｓ）及其用途（一）

Legal Events

Date Code Title Description
PC1 Assignment before grant (sect. 113)

Owner name: SEATTLE GENETICS, INC.

Free format text: FORMER APPLICANT(S): BAYER INTELLECTUAL PROPERTY GMBH; BAYER PHARMA AKTIENGESELLSCHAFT

MK5 Application lapsed section 142(2)(e) - patent request and compl. specification not accepted